The hot peppers from the species Capsicum annuum L., C. frutesscens L. and C. minimum L. have been consumed as food by mankind for some periods of time. The active ingredient, 8-methyl-N-vanillyl-6-nonenamide (capsaicin), was isolated and identified by Nelson. (Nelson, E. K., J. Am. Chem. Soc. 45, 2179-2181, (1923).) and here after studies concerning its physiological and pharmacological effects on animals had been carried out. Skofitsch (Skofitsch, G. Donnerer, J. Petronijevic, S., Saria, A., and Lembeck, F., Naunyn-Schmiedebergs Arch. Pharmacol. 322, 153-157, 1983.) showed that capsaicin can selectively activate the vagal C-fiber afferents in the airways and can also stimulate the central nervous system (CNS) and the local reflex systems to release some biologically active peptides. Lundberg (Lundberg, J. M., Brodin E., and Saria, A., Acta. Physiol. Acand., 119, 243-252, (1983).) found out that when the compound was sprayed on the respiratory organ of the animal, it can cause the release of substance P and CGRP (calcitonin gene related peptide) of the airways. When the mucus of the experimental felines were treated with capsaicin, local mucosal bleeding was observed via the stimulation of the C-fiber afferents. These agents were also observed to increase the permeability of blood vessels so as to cause the extravasation of proteins. Later researches in this area (Toh, C. C., Lee, T. S., and Kiang, A. K., Brit. J. Pharmacol., 10, 175-182, (1955), Coleridge, H. M., Coleridge, J. C., and Kidd, C., J. Physiol., London, 170, 272-285, (1964), Virus, R. M., and Gebhart, G. F., Life Sci., 25, 1273-1284, (1979).) indicate that capsaicin has overt effects in the dilation of the aorta, lowering the blood pressure and slowing down the heart rate.
Recent studies in the biochemistry of capsaicin show that it can enhance the activity of hormone sensitive lipase (HSL) in fatty tissues but can inhibit the activities of Ca.sup.2+, calmodulin dependent cyclic AMP and phosphodiesterase (PDE) in adipose tissues. As a result of these lipolytic activity, it can also be used to lower the lipid level in blood. Further more capsaicin was also found to inhibit the aggregation of blood platelets. Even though many pharmacological researches confirm the effects of capsaicin on the cardiovasular system, its properties as a potent stimulant (spicy sensation even at a 1/8000 mg concentration) and as a neurotoxic agent (extravasation of peptides, airways smooth muscle contraction) coupled with the fact that it is only sparingly soluble in water have greatly retarded the efforts towards developing the compound as a clinically useful agent. As long as concerning of improving its aqueous solubility, solvents such as: alcohols, DMSO and Tween 80 had been employed; but all these had shown to affect its natural pharmacological profile. The intent of the present invention is to introduce a hydrophilic moeity to the structure so as to improve its water soluble property. The followings are the detail disclosure of the invention.